ArticleCommunications biology2022
Identification of SARS-CoV-2 inhibitors targeting Mpro and PLpro using in-cell-protease assay.
Article in Communications biology, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 107 papers.
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Who cites it
107 citing papers in PubMed.
- Preventive and therapeutic benefits of nelfinavir in rhesus macaques and human beings infected with SARS-CoV-2.Signal transduction and targeted therapy · 2023Trial
- Identification of Potential SARS-CoV-2 Main Protease (MPro) Inhibitors Through Pharmacophore Modeling, Molecular Docking, and Molecular Dynamics Simulation Approaches.International journal of molecular sciences · 2026Article
- Cross-Family Mechanistic Analysis of Plant Alkaloids Against Neglected Arboviruses and Related RNA Viruses.Molecules (Basel, Switzerland) · 2026Review
- Selected Cannabinoids, Cannabimimetic Agents andPharmaceuticals (Basel, Switzerland) · 2026Review
- Integrated Evaluation ofPharmaceuticals (Basel, Switzerland) · 2026Article
- Lycorine Derivative Inhibits SARS-CoV-2 Replication by Reducing -1 Programmed Ribosomal Frameshifting via Targeting ZAP.MedComm · 2026Article
- Metabolites from South African Medicinal Plants as Dual-Function Inhibitors of the SARS-CoV-2 Papain-like Protease (PLLife (Basel, Switzerland) · 2026Article
- Development of a Complementation Assay to Monitor Pan-Coronavirus 3C-like Protease Activity.Viruses · 2026Article
- Natural Alkaloids as Antiviral Agents Against RNA Viruses: A Comprehensive and Mechanistic Review.Molecules (Basel, Switzerland) · 2026Review
- Design, synthesis and activity evaluation of dual-target inhibitors against papain-like and main proteases of porcine epidemic diarrhea virus.Journal of advanced research · 2026Article
- Coupling high-throughput protease enzymology with viral replication reveals biochemical constraints of viral fitness.bioRxiv : the preprint server for biology · 2026Article
- Affinity of drug candidates binding to SARS-CoV-2 PLpro assessed using a generalized-ensemble method.Scientific reports · 2026Article
- Identification of a Quinolone-Based Scaffold as a Dual SARS-COV-2 PLᵖʳᵒ and Mᵖʳᵒ Inhibitor: An Integrated Molecular Modeling and In-vitro Evaluation Approach.Drug design, development and therapy · 2026Article
- A Novel Fluorescence Polarization Binding Assay for the Main Protease (MACS pharmacology & translational science · 2025Article
- SARS-CoV‑2 Papain-Like Protease Inhibitors Based on Naphthalen-1-ylethanamine and Halogenated Benzene Moieties.ACS omega · 2025Article
- Discovery of broad-spectrum antivirals targeting viral proteases using in silico structural modeling and cellular analysis.Antiviral research · 2025Article
- Optimized pipeline and designer cells for synthetic-biology-based high-throughput screening of viral protease inhibitors.Cell reports methods · 2025Article
- Computational Evaluation and Multi-Criteria Optimization of Natural Compound Analogs Targeting SARS-CoV-2 Proteases.Current issues in molecular biology · 2025Article
- Molecular Recognition of SARS-CoV-2 Mpro Inhibitors: Insights from Cheminformatics and Quantum Chemistry.Molecules (Basel, Switzerland) · 2025Article
- Review
47 more citing papers are in PubMed but not listed here.
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Authors and funding
9 authors.
Funding
Abstract
SARS-CoV-2 proteases Mpro and PLpro are promising targets for antiviral drug development. In this study, we present an antiviral screening strategy involving a novel in-cell protease assay, antiviral and biochemical activity assessments, as well as structural determinations for rapid identification of protease inhibitors with low cytotoxicity. We identified eight compounds with anti-SARS-CoV-2 activity from a library of 64 repurposed drugs and modeled at protease active sites by in silico docking. We demonstrate that Sitagliptin and Daclatasvir inhibit PLpro, and MG-101, Lycorine HCl, and Nelfinavir mesylate inhibit Mpro of SARS-CoV-2. The X-ray crystal structure of Mpro in complex with MG-101 shows a covalent bond formation between the inhibitor and the active site Cys145 residue indicating its mechanism of inhibition is by blocking the substrate binding at the active site. Thus, we provide methods for rapid and effective screening and development of inhibitors for blocking virus polyprotein processing as SARS-CoV-2 antivirals. Additionally, we show that the combined inhibition of Mpro and PLpro is more effective in inhibiting SARS-CoV-2 and the delta variant.
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